Vicriviroc Malate |
| Katalog-Nr.GC17920 |
CCR5 antagonist, orally active, second generation
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 541503-81-5
Sample solution is provided at 25 µL, 10mM.
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Vicriviroc is an inhibitor of CCR5 signaling with IC50 value of 0.91nM [1].
The first step of HIV-1 infection is that the viral envelope, gp120, will interact with cellular coreceptor CCR5. As a second CCR5 antagonist, Vicriviroc can block this interaction and has the antivirus potency. In the chemotaxis assay, Vicriviroc can innhibit chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human CCR5 with IC50 value below 1 nM. In the calcium flux assay, Vicriviroc inhibit intracellular calcium release induced by receptor stimulation. Vicriviroc is also proved to inhibit GTPgammaS binding induced by RANTES with mean IC50 of 4.2±1.3nM in a GTPgammaS exchange assay. In a PBMC infection assay with 30 R5-tropic HIV-1 isolates, Vicriviroc potently inhibits all the viral isolates with geometric mean EC50s ranging between 0.04 nM and 2.3 nM. Activity of vicriviroc against drug-resistant viruses has also been tested. Vicriviroc is effective against all the viruses with defined RTI, PRI, or fusion inhibitor resistance patterns. Furthermore, engineered viruses containing mutations in the gp41 gene associated with enfuvirtide resistance are completely sensitive to vicriviroc. So far, Vicriviroc has shown good tolerance and partial therapeutic success in phase II clinical trials for HIV [1,2].
References:
[1] Julie M. Strizki, Cecile Tremblay, Serena Xu, Lisa Wojcik , Nicole Wagner, Waldemar Gonsiorek, R. William Hipkin, Chuan-Chu Chou, Catherine Pugliese-Sivo, Yushi Xiao, Jayaram R. Tagat, Kathleen Cox, Tony Priestley, Steve Sorota, Wei Huang, Martin Hirsch, Gregory R. Reyes and Bahige M. Baroudy. Antimicrobial Agents and Chemotherapy. 2005, 49(12):4911-4919.
[2] Marco Velasco-Velázquez, Xuanmao Jiao, Marisol De La Fuente, et al. CCR5 Antagonist Blocks Metastasis of Basal Breast Cancer Cells. Cancer Research. 2012 (72): 3839-3850.
| Cas No. | 541503-81-5 | SDF | |
| Chemical Name | (4,6-dimethylpyrimidin-5-yl)-[4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methylpiperazin-1-yl]-4-methylpiperidin-1-yl]methanone;2-hydroxybutanedioic acid | ||
| Canonical SMILES | CC1CN(CCN1C(COC)C2=CC=C(C=C2)C(F)(F)F)C3(CCN(CC3)C(=O)C4=C(N=CN=C4C)C)C.C(C(C(=O)O)O)C(=O)O | ||
| Formula | C28H38F3N5O2.C4H6O5 | M.Wt | 667.72 |
| Löslichkeit | ≥ 18mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4976 mL | 7.4882 mL | 14.9763 mL |
| 5 mM | 0.2995 mL | 1.4976 mL | 2.9953 mL |
| 10 mM | 0.1498 mL | 0.7488 mL | 1.4976 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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